Synthesis and enzyme inhibitory activities of a series of lipidic diamine and aminoalcohol derivatives on cytosolic and secretory phospholipases A2
✍ Scribed by Rut Lucas; Amalia Úbeda; Miguel Payá; Mario Alves; Esther del Olmo; José L. López; Arturo San Feliciano
- Publisher
- Elsevier Science
- Year
- 2000
- Tongue
- English
- Weight
- 134 KB
- Volume
- 10
- Category
- Article
- ISSN
- 0960-894X
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✦ Synopsis
We have synthesised some lipidic diamines and aminoalcohols and examined their behaviour as inhibitors of secretory and cytosolic PLA2. Some structure-activity relationships considerations have been deduced. Compound 14 was a potent and selective inhibitor of cPLA2 and compound 4 showed a dual inhibitory profile against both types of PLA2 while no cytotoxicity at 10 microM on human neutrophils or on murine macrophage line was observed for both.
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